Search Results - "Grözinger, Karl G."

Efficient synthesis of α-fluoromethylhistidine di-hydrochloride and demonstration of its efficacy as a glutathione S-transferase inhibitor by Considine, Kelly L., Stefanidis, Lazaros, Grozinger, Karl G., Audie, Joseph, Alper, Benjamin J.

“…[Display omitted] Histidine decarboxylase (HDC) is an enzyme that converts histidine to histamine. Inhibition of HDC has several medical applications, and HDC…”
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Inhibition of human leukocyte elastase (HLE) by N-substituted peptidyl trifluoromethyl ketones by Skiles, Jerry W, Fuchs, Victor, Miao, Clara, Sorcek, Ronald, Grozinger, Karl G, Mauldin, Scott C, Vitous, Jana, Mui, Philip W, Jacober, Stephen

“…A series of tripeptides possessing trifluoromethyl or aryl ketone residues at P1 were prepared and evaluated both in vitro and in vivo as potential inhibitors…”
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A novel stereoselective route to (S)-(+)-.alpha.-(fluoromethyl)histidine: .alpha.-halomethylation of (2R,4S)-3-benzoyl-2-(1,1-dimethylethyl)-1-methyl-4-[(N-tritylimidazol-4-yl)methyl]-1,3-imidazolidin-5-one. Synthesis and proton NMR spectroscopy by Grozinger, Karl G, Kriwacki, Richard W, Leonard, Scott F, Pitner, T. Phil

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Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 1. Tricyclic pyridobenzo- and dipyridodiazepinones by Hargrave, Karl D, Proudfoot, John R, Grozinger, Karl G, Cullen, Ernest, Kapadia, Suresh R, Patel, Usha R, Fuchs, Victor U, Mauldin, Scott C, Vitous, Jana

“…Novel pyrido[2,3-b][1,4]benzodiazepinones (I), pyrido[2,3-b][1,5]benzodiazepinones (II), and dipyrido[3,2-b:2',3'-e][1,4]diazepinones (III) were found to…”
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Novel Non-nucleoside Inhibitors of Human Immunodeficiency Virus Type 1 (HIV-1) Reverse Transcriptase. 4. 2-Substituted Dipyridodiazepinones as Potent Inhibitors of Both Wild-Type and Cysteine-181 HIV-1 Reverse Transcriptase Enzymes by Proudfoot, John R, Hargrave, Karl D, Kapadia, Suresh R, Patel, Usha R, Grozinger, Karl G, McNeil, Daniel W, Cullen, Ernest, Cardozo, Mario, Tong, Liang

“…The major cause of viral resistance to the potent human immunodeficiency virus type 1 reverse transcriptase (RT) inhibitor nevirapine is the mutation…”
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Synthesis of imidazo[5,4-d] [1,3]thiazines: X-ray structure of N-methyl-N′-[5-(methylamino)-3-nonylimidazo[5,4-d] [1,3]thiazin-7(3H)-ylidene]thiourea by Grözinger, Karl G., Onan, Kay D.

“…N‐Alkyl‐N′‐[5‐(alkylamino)‐3‐alkylimidazo[5,4‐d] [1,3]thiazin‐7(3H)‐ylidene]thioureas were obtained by the reaction of 1‐substituted 5‐amino‐4‐cyanoimidazoles…”
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Syntheses and reactions of some 1-substituted-7-alkyl-2-thioxopurines: X-Ray structure of 6-methylamino-7-nonyl-2-thioxopurine by Grözinger, Karl G., Onan, Kay D.

“…Several 1‐substituted‐7‐alkyl‐2‐thioxopurines 8,9,10 were synthesized by the reaction of isothiocyanates with 1‐alkyl‐4‐amino‐5‐cyanoimidazoles 3. Treatment of…”
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Synthesis of five nevirapine metabolites by Grozinger, Karl G., Byrne, Denis P., Nummy, Laurence J., Ridges, Michael D., Salvagno, Annette

“…Nevirapine (1) is a non‐nucleoside reverse transcriptase inhibitor marketed for HIV treatment by Boehringer Ingelheim as Viramune® since 1996. In vitro studies…”
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